Teicoplanin (Tei) is a glycopeptide antibiotic that has bactericidal activity against Gram positive aerobic and anaerobic bacteria. It inhibits the growth of susceptible organisms by interfering with the biosynthesis of the cell-wall at a site different from that affected by beta-lactam antibiotics. Teicoplanin is a mixture of glycopeptide components which, on the basis of high performance liquid chromatography (HPLC) separation, are currently classified into six main subcomponents (as individual or as a group) according to their alkyl side chain and therefore by their polarity in elution in the referenced chromatographic system.
Bacteria have the ability to generate resistance to antibiotics through lateral gene transfer, mutation of enzymes, or the expression of enzymes which actively pump the antibiotic out of the cell or break it down. Over the past 10 years, resistance to existing antibiotics has become a significant problem. In practice, strains such as methicillin-resistant Staphylococcus Aureus (MRSA), methicillin-resistant Staphylococcus Epidermidis (MRSE), penicillin-resistant Streptococcus pneumonia, quinolone-resistant Staphylococcus Aureus (QRSA), vancomycin-resistant Staphylococcus Aureus (VRSA), vancomycin-resistant Enterococci (VRE), and multi-drug resistant Mycobacterium tuberculosis show resistance to most antibiotics in use. Glycopeptide is generally the last line antibiotic to treat multidrug-resistant gram-positive pathogens MRSA and VRE. This class of antibiotics is empowered by the N-acyltransferase, attaching a long aliphatic chain on the glucosamine moiety at the central residue of glycopeptide pseudoaglycone. Thus, it is urgently demanded to develop new antibiotics and new mechanism of action to treat and/or prevent bacterial infections, in particular, to overcome the bacterial resistance problem.